The compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, was disclosed for the first time in EP Patent No. 0000338 and has the molecular structure depicted below.

Gaboxadol is a GABAA receptor agonist with functional selectivity for the delta containing GABAA receptor. Gaboxadol has been suggested for use in treating a variety of neurological and psychiatric disorders such as epilepsy, Parkinson's disease, schizophrenia and Huntington's chorea. WO 97/02813 discloses the use of gaboxadol for treatment of sleep disorders, and positive results have been obtained in pre-clinical models of depression (WO 2004/112786).
Gaboxadol may be prepared using methods that are well known in the art. EP 0000338 and Krogsgaard-Larsen, Acta Chem. Scand. B, (1977), 31: 584-588 disclose a process wherein gaboxadol is prepared from ethyl-1-benzyl-3-oxopiperidine-4-carboxylate. Rong and Chang, Chin. J. Med. Chem. (2007), 17:166-169 disclose a process for manufacture of gaboxadol starting from glycine ester hydrochloride, benzyl chloride and -butyrolactone. WO 2005/023820 discloses a process for manufacture of gaboxadol from 3,N-Dihydroxy-isonicotinamide as starting material via the intermediate isoxazolo 5,4-c pyridin-3-ol (HIP).
There is a need for a superior alternative to the current manufacturing processes of gaboxadol with respect to parameters such as cost-effectiveness, safety, robustness and applicability for industrial scale.